GSK3145095
GSK3145095 is a potent and orally active RIPK1 inhibitor (IC50 = 5 nM) with potential antineoplastic and immunomodulatory activities. GSK3145095 disrupts RIPK1-mediated signaling, which may reduce C-X-C motif chemokine ligand 1 (CXCL1)-driven recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME). This allows effector cells, such as natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), to kill and eliminate cancer cells. GSK3145095 is currently under clinical trails.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | GSK3145095 |
|---|---|
| Iupac 化学名称 | (S)-5-benzyl-N-(7,9-difluoro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-4H-1,2,4-triazole-3-carboxamide |
| 同义词 | GSK3145095; GSK-3145095; GSK 3145095; |
| 英文同义词 | GSK3145095; GSK-3145095; GSK 3145095; |
| 分子式 | C20H17F2N5O2 |
| 分子量 | 397.3858 |
| Smile | O=C(C1=NN=C(CC2=CC=CC=C2)N1)N[C@H]3CCC4=CC(F)=CC(F)=C4NC3=O |
| InChiKey | ATQAGKAMBISZQM-HNNXBMFYSA-N |
| InChi | InChI=1S/C20H17F2N5O2/c21-13-9-12-6-7-15(19(28)25-17(12)14(22)10-13)23-20(29)18-24-16(26-27-18)8-11-4-2-1-3-5-11/h1-5,9-10,15H,6-8H2,(H,23,29)(H,25,28)(H,24,26,27)/t15-/m0/s1 |
| Cas号 | 1622849-43-7 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer
Philip A. Harris, Jill M. Marinis, John D. Lich, Scott B. Berger, Anirudh Chirala, Julie A. Cox, Patrick M. Eidam, Joshua N. Finger, Peter J. Gough, Jae U. Jeong, James Kang, Viera Kasparcova, Lara K. Leister, Mukesh K. Mahajan, George Miller, Rakesh Nagilla, Michael T. Ouellette, Michael A. Reilly, Alan R. Rendina, Elizabeth J. Rivera, Helen H. Sun, James H. Thorpe, Rachel D. Totoritis, Wei Wang, Dongling Wu, Daohua Zhang, John Bertin, and Robert W. Marquis
Publication Date (Web): May 9, 2019 (Featured Letter)
DOI: 10.1021/acsmedchemlett.9b00108
